In vitroactivity of compounds isolated fromPiper crassinerviumagainstTrypanosoma cruzi

Lopes, Adriana A.; López, Silvia N.; Regasini, Luís Octávio; Batista, João M.; Ambrósio, Daniela Luz; Kato, Massuo Jorge; Bolzani, Vanderlan da Silva; Cicarelli, Regina Maria Barretto; Furlan, Maysa

doi:10.1080/14786410802243271

Cited by 24 publications

(10 citation statements)

References 18 publications

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“…A dose dependent decrease in parasite growth was evident within 2 days of addition of BZ to cultures and was clearly evident throughout the remainder of the 4 day assay period (Figure 3A). The IC 50 calculated for benznidazole is similar to that of other methods, including visual counting (Figure 3A), and as previously reported in the literature for several T. cruzi strains [40]–[41]. This method showed low intra-assay variation and a very good consistency by the inter-assay analysis (Figures 3B).…”

Section: Resultssupporting

confidence: 85%

In Vitro and In Vivo High-Throughput Assays for the Testing of Anti-Trypanosoma cruzi Compounds

et al. 2010

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BackgroundThe two available drugs for treatment of T. cruzi infection, nifurtimox and benznidazole (BZ), have potential toxic side effects and variable efficacy, contributing to their low rate of use. With scant economic resources available for antiparasitic drug discovery and development, inexpensive, high-throughput and in vivo assays to screen potential new drugs and existing compound libraries are essential.MethodsIn this work, we describe the development and validation of improved methods to test anti-T. cruzi compounds in vitro and in vivo using parasite lines expressing the firefly luciferase (luc) or the tandem tomato fluorescent protein (tdTomato). For in vitro assays, the change in fluorescence intensity of tdTomato-expressing lines was measured as an indicator of parasite replication daily for 4 days and this method was used to identify compounds with IC50 lower than that of BZ.FindingsThis method was highly reproducible and had the added advantage of requiring relatively low numbers of parasites and no additional indicator reagents, enzymatic post-processes or laborious visual counting. In vivo, mice were infected in the footpads with fluorescent or bioluminescent parasites and the signal intensity was measured as a surrogate of parasite load at the site of infection before and after initiation of drug treatment. Importantly, the efficacy of various drugs as determined in this short-term (<2 weeks) assay mirrored that of a 40 day treatment course.ConclusionThese methods should make feasible broader and higher-throughput screening programs needed to identify potential new drugs for the treatment of T. cruzi infection and for their rapid validation in vivo.

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Section: Resultssupporting

confidence: 85%

In Vitro and In Vivo High-Throughput Assays for the Testing of Anti-Trypanosoma cruzi Compounds

et al. 2010

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“…For this reason, there is a need for new antifungal compounds which can serve as lead compounds for further development in antifungal chemotherapy. In this way, plants have been proven to be a rich source of antimicrobial agents (Vieira et al, 2005, Alves et al, 2006Dias et al, 2006;Sena Filho et al, 2006;Oliveira et al, 2007;Batista-Júnior et al, 2008;Cardoso-Lopes et al, 2008;Lopes et al, 2008;Tempone et al, 2008;Bertucci et al, 2009;Costa et al, 2009;Regasini et al, 2009a;Silva-Júnior et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

Antimicrobial activity of Pterogyne nitens Tul., Fabaceae, against opportunistic fungi

Regasini¹,

Pivatto

Scorzoni³

et al. 2010

Rev. bras. farmacogn.

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RESUMO: "Atividade antimicrobiana de Pterogyne nitens Tul., Fabaceae, contra fungos oportunistas". No contexto de nossas pesquisas por novos agentes antifúngicos obtidos da flora brasileira, oito extratos e doze frações de Pterogyne nitens Tul., Fabaceae, foram submetidos ao ensaio antifúngico pelo método de microdiluição, contra quatro espécies de fungos oportunistas, Candida albicans, Candida krusei, Candida parapsilosis e Cryptococcus neoformans. Este trabalho revelou que os extratos e frações de P. nitens foram mais ativos contra C. krusei e C. parapsilosis quando comparados a C. neoformans, sendo que o crescimento de C. albicans foi moderadamente afetado por todos os extratos e frações. As atividades mais potentes foram observadas para as frações n-butanólica dos galhos (CIM = 15,6 µg/mL) e raízes (CIM = 31,2 µg/mL) contra C. krusei. Adicionalmente, a fração n-butanólica dos galhos foi submetida ao fracionamento cromatográfico, resultando no isolamento de quatro alcaloides guanidínicos, sendo N-1,N-2,N-3-triisopentenilguanidina (1), descrito pela primeira vez em espécies da família Fabaceae e nitensidinas A-C (2-4), os quais apresentaram atividade antifúngica moderada contra C. krusei (CIM = 62,5 µg/ mL) e C. parapsilosis (CIM = 31,2 µg/mL). Unitermos:Pterogyne nitens, alcaloides guanidínicos, antifúngico, fungos oportunistas, Candida spp., Cryptococcus neoformans. ABSTRACT:As part of our ongoing research on antifungal agents from Brazilian flora, eight extracts and twelve fractions from Pterogyne nitens Tul., Fabaceae, were screened for antimicrobial activity against four opportunistic fungi species (Candida albicans, Candida krusei, Candida parapsilosis and Cryptococcus neoformans) using a broth microdilution method. The present investigation reveals that P. nitens extracts and fractions were more effective against C. krusei and C. parapsilosis than against C. neoformans. The growth of C. albicans was moderately affected by all tested extracts and fractions. The strongest effects were observed for n-butanol fractions from branches (MIC = 15.6 µg/mL) and roots (MIC = 31.2 µg/mL) against C. krusei. Additionally, the chromatographic fractionation of the n-butanol fraction from branches afforded four guanidine alkaloids; N-1,N-2,N-3-triisopentenylguanidine (1), described for the first time in the Fabaceae family, and nitensidines A-C (2-4), which showed moderate activity towards C. krusei (MIC = 62.5 µg/mL) and C. parapsilosis (MIC = 31.2 µg/mL).

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“…Continuing our studies on the discovery of trypanocidal agents obtained from plants from both the Cerrado and the Atlantic Forest Lopes et al, 2008;Regasini et al 2009), 92 ethanol extracts of species belonging to the families Annonaceae, Apiaceae, Cucurbitaceae, Lamiaceae, Lauraceae, Moraceae, Nyctaginaceae, and Verbenaceae were tested against epimastigote forms of Trypanosoma cruzi (Y and Bolivia strains), and their cytotoxic activity on LLCMK 2 fibroblasts was evaluated. The emergency to find new antiprotozoal agents with trypanocidal activity and the evidence that some species of the aforementioned families have trypanocidal activity against parasitic forms of T. cruzi provided the motivation to carry out the screening of such extracts (Buainain et al, 1992;Fournet et al, 2007;Osorio et al, 2007;Cabral et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

Trypanocidal activity of Brazilian plants against epimastigote forms from Y and Bolivia strains of Trypanosoma cruzi

Alves¹,

Regasini²,

Funari³

et al. 2012

Rev. bras. farmacogn.

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Abstract:Chagas disease is one of the main public health problems in Latin America. Since the available treatments for this disease are not effective in providing cure, the screening of potential antiprotozoal agents is essential, mainly of those obtained from natural sources. This study aimed to provide an evaluation of the trypanocidal activity of 92 ethanol extracts from species belonging to the families Annonaceae, Apiaceae, Cucurbitaceae, Lamiaceae, Lauraceae, Moraceae, Nyctaginaceae, and Verbenaceae against the Y and Bolivia strains of Trypanosoma cruzi. Additionally, cytotoxic activity on LLCMK2 fi broblasts was evaluated. Both the trypanocidal activity and cytotoxicity were evaluated using the MTT method, in the following concentrations: 500, 350, 250, and 100 µg/mL. Benznidazole was used for positive control. The best results among the 92 samples evaluated were obtained with ethanol extracts of Ocotea paranapiacabensis (Am93) and Aegiphila lhotzkiana (Am160). Am93 showed trypanocidal activity against epimastigote forms of the Bolivia strain and was moderately toxic to LLCMK2 cells, its Selectivity Index (SI) being 14.56, while Am160 showed moderate trypanocidal activity against the Bolivia strain and moderate toxicicity, its SI being equal to 1.15. The screening of Brazilian plants has indicated the potential effect of ethanol extracts obtained from Ocotea paranapiacabensis and Aegiphila lhotzkiana against Chagas disease.

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In vitroactivity of compounds isolated fromPiper crassinerviumagainstTrypanosoma cruzi

Cited by 24 publications

References 18 publications

In Vitro and In Vivo High-Throughput Assays for the Testing of Anti-Trypanosoma cruzi Compounds

In Vitro and In Vivo High-Throughput Assays for the Testing of Anti-Trypanosoma cruzi Compounds

Antimicrobial activity of Pterogyne nitens Tul., Fabaceae, against opportunistic fungi

Trypanocidal activity of Brazilian plants against epimastigote forms from Y and Bolivia strains of Trypanosoma cruzi

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